Plevitrexed(Synonyms: ZD 9331; BGC9331)

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Plevitrexed (Synonyms: ZD 9331; BGC9331)

Plevitrexed (ZD 9331; BGC9331) 是口服有效的胸苷酸合酶 (TS) 抑制剂，Ki 值为 0.44 nM。Plevitrexed 通过 α-叶酸受体以及还原的叶酸载体吸收。Plevitrexed 有用于胃癌的潜力。

Plevitrexed(Synonyms: ZD 9331; BGC9331)

Plevitrexed Chemical Structure

CAS No. : 153537-73-6

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生物活性

Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical[1][2][3].

体外研究
(In Vitro)

ZD9331 inhibits the transport of [3H]-methotrexate into L1210 and W1L2 cells with a Ki of∼1 µM[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

532.53

Formula

C26H25FN8O4
CAS 号

153537-73-6
中文名称

普来曲塞
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Tochowicz A, et al. Development and binding mode assessment of N-[4-[2-propyn-1-yl[(6S)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta[g]quinazolin-6-yl]amino]benzoyl]-l-γ-glutamyl-D-glutamic acid (BGC 945), a novel thymidylate synthase inhibitor that targets tumor cells. J Med Chem. 2013 Jul 11;56(13):5446-55.

    [2]. A. Thomas, et al. A phase I/II study of plevitrexed with nutritional vitamin supplementation in gastric cancer.

    [3]. Marsham PR, et al. Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors. J Med Chem. 1999 Sep 23;42(19):3809-20.

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